The New Era of Energy – Powerhouse Combo: Caffeine + Lithium Orotate

It’s no secret that caffeine is the most widely consumed stimulant on the market today. At the correct dosage, it’s relatively safe to be taken daily (multiple times for some) for the extra oomph and wakefulness it provides. Typically, you’ll find that energy enhancement falls into the following categories, which are also listed sequentially:

Naturally caffeinated beverages such as coffee and tea.

Caffeinated soft and energy drinks, these include common mixtures which have been around since the late 90’s, typically a cocktail comprising of caffeine, sugar, b-vitamins, and compounds that play on neurotransmitters / monoamines such as choline donors, tyrosine, and taurine.

More recently, you’ll find energy enhancing supplements / consumables combining caffeine with compounds from bullet 2, along with other safe nootropics, such as bacopa, rhodiola, and theanine.

Let’s take a moment to understand how we got to where we are today.

Starting with the first bullet, these are drinks that we’ve all become accustomed to. Coffee and tea both offer a brief, warm and tasty time-out from the activities of our daily routine. Sipping away, while slowing your pace to enjoy these beverages has become the staple of our mornings.

Coffee, for example, has other natural compounds found within it which benefit the consumer, such as antioxidants (which degrade when the beans are roasted dark) [R1]. Chlorogenic acid (CGA), another compound that also has been shown, in the rat model, to promote neuroprotective effects by slightly inhibiting acetyl cholinesterase, the enzyme that breaks down beneficial neurotransmitter acetylcholine[R2]. The average serving of coffee contains anywhere from 100 to 150mg of caffeine.

Tea is still the primary source of caffeine consumption in many parts of the world. Black tea typically contains anywhere from 30 to 60mg of caffeine and possesses many other beneficial compounds such as heart healthy flavonoids, polyphenols, and catechins (such as EGCG, though this compound is more prevalent in green tea). Black tea also contains a unique amino acid, L-theanine, which has been shown to increase alpha wave brain activity; this is tied to a relaxed state [R3]. However, the amount found in a serving of black tea may not be enough at ~20mg, the effective dose varies greatly between individuals, typically ranging anywhere from 50 to 200mg; anecdotally users aim for a 2:1 ratio of theanine to caffeine.

Frankly speaking, both drinks, when consumed in moderation offer some incredible benefits. The risk comes when larger amounts are consumed. Put plainly, caffeine is a stimulant [enabler], gone unabated it can lead to anxiety, jitters, difficulties concentrating, higher blood pressure, and dependency. Unfortunately, coffee does not contain compounds to prevent these types of effects and though tea does have theanine, it is not enough to balance out the sides of excess caffeine consumption.

Onto bullet 2, these are the common energy drinks across the market. They are not at all humble in their marketing, making it glaringly obvious of their intentions. The difference here is that they are not your go-to warm comfort drink, e.g. you probably won’t meet a business partner at an energy drink shop as you would say a coffee house. These drinks take the energy, alertness, and wakefulness model and add to it. Some of the most potent products out there for their intended use, however they boast the same vice as coffee and tea. There really aren’t any compounds to balance out the powerful energy combinations found within these drinks, except maybe taurine, which has been shown to have relaxing properties[R4]. However, this ‘relaxation’ may also worsen the crash that commonly follows caffeine consumption.

Furthermore, most of the compounds found in these drinks promote additional energy and wakefulness, beyond that of caffeine alone. Compounds like the amino acid tyrosine (dopamine precursor) and citicoline (choline donor) promote neurotransmitters which may intensify the effects of caffeine. For consumers sensitive to this, increased anxiety, higher blood pressure and subsequent headaches may potentially become an issue. Most folks regulate this by limiting the amount consumed per serving, e.g. not finishing the whole can.

Let’s move on to bullet 3. The latest buzz within the market are nootropics, though there has been a community using [experimenting with] these compounds for years, only recently has there been an explosion onto the mainstream. You’ll see them being marketed on social media, message boards, reddit etc. Essentially, a nootropic is a cognitive/memory/creativity boosting compound that is reportedly safe to consume at the recommended dosages. The term itself is a bit nebulous, I’ve seen disagreements ranging from calling caffeine or nicotine a ‘true’ nootropic to similar discussions around prescription medications.

I’ve benefited significantly myself from use of such compounds and attribute this primarily to combining the right compounds at the most effective dosages.

Caffeine at a Glance

Let’s dive right into this, the ‘right compounds at the most effective dosages’. Starting with caffeine, benefits include:

Reduces fatigue and improves wakefulness

Improves reaction time and promotes alertness

Improves athletic performance and output

The mode of action is linked to the similarities between the caffeine molecule and adenosine. Adenosine, amongst many other functions, plays an important role in energy transfer and acts like a neuromodulator in that it promotes sleep when enough of it binds to specific receptors in the brain. I liken its function promoting sleep to the following metaphor: Think of a bouncer counting the number of people entering a lounge, he is required to shut the doors once a certain number (or ratio) is reached. When it comes to sleep, once enough adenosine binds to receptors within the brain, your body tells you it’s time for bed.

Being that caffeine is so similar to adenosine, at least to the body, it binds to the same receptors preventing adenosine to do so; known as antagonism of the adenosine receptor. Therefore, the sleepiness is avoided. However, caffeine elicits other effects, such as plasma increases of epinephrine (adrenaline), norepinephrine (noradrenaline) [R5]; the former of which is part of the fight-of-flight stress response cascade. As you may have noted from my previous anxiety article, this response, when constantly activated leads to profound levels of anxiety and anxious behavior. Known commonly in the caffeine consuming community as the jitters, edgy, even irritability.

Glutamate is another excitatory neurotransmitter that is affected by caffeine consumption. Specifically, by binding to the adenosine receptor, neurons fire faster causing your brain to release excess glutamate in response. This is helpful for learning, however can be severely detrimental if excess glutamate causes excitotoxicity, leading to neuron damage. As you may have guessed, it also promotes anxiety, which in turn leads to learning impairment. Balance is key, you want to maintain optimal concentrations of the neurotransmitter to stay in a peak state. To do this, I recommend synergistic compounds.

Lithium Orotate + Caffeine: Be more effective with this Energy Powerhouse

Elemental Lithium has had an interesting past when it comes to its use in psychiatry. Dating to Ancient Greece, it was said that physician Soranus had used alkaline salt baths high in lithium to treat mania and melancholia (depression). More recently, it’s use in psychiatry was established by Dr. Cade from Australia. As a former WWII prisoner of war, he had accidentally discovered that lithium has pronounced effect on mania; I say accidentally because he thought mania was linked to a metabolic disorder due to excess urea in patient urine. Subsequently, he had injected lithium urate into guinea pigs and found that it had a calming effect.

This started the use of lithium as an extremely effective treatment for manic depressants, bipolar disorder, and anxiety to name a few ailments. Prescription lithium is typically found in the form Lithium Carbonate and is prescribed in dosages starting at 300mg all the way up to 1800mg daily. It is important to note that you are consuming anywhere from 60mg to 360mg of elemental lithium respectively. At these large dosages you may lower thyroid function or negatively impact kidney function.

However, it is particularly important to note that prescription lithium differs greatly from the over-the-counter form, known as lithium orotate. Lithium orotate has elemental lithium bound to orotic acid; orotates are mineral salts of orotic acid, they are commonly found in nature and in our bodies. In the 1970’s, Dr. Nieper of Germany had discovered that mineral bound orotates (such as magnesium and lithium orotate) can pass through cell membranes intact without disassociating into the component ions. This allowed the molecule to bring (e.g. deliver) the ion to specific membrane sites within the cell. Therefore, Lithium Orotate may be a much more effective and safer alternative to prescription lithium; it may pass the blood brain barrier intact, essentially requiring significantly less elemental lithium (typically starting at ~5mg) to get the same job done. Sounds much better than the other, brute force loading method now doesn’t it?

The point is that you may elicit the same benefits, such as the following:

It’s important to note that both lithium orotate and caffeine offer a multitude of benefits, but it’s the combination of the two that offers significant advantages over consuming caffeine alone. Lithium orotate promotes an anxiolytic effect by balancing out the impact of excessive glutamate and epinephrine (adrenaline). These two neurotransmitters are primary contributors to anxiety, nervousness, and irritability; by modulating them, lithium orotate sets the foundation for a much more pleasant and manageable energy surge than that of caffeine alone.

Furthermore, there is also the benefit of increased dopamine and serotonin[R8] in specific regions of the brain, both which can positively affect your mood. The combination of energy + good mood is critical, because lacking either of those negates the other. Anecdotally, this combo has worked wonders in my day-to-day performance, patience, and well-being.

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